CHICAGO, June 2 /PRNewswire-FirstCall/ -- Exelixis, Inc. (Nasdaq: EXEL)
reported data from three clinical trials of XL647, a novel small molecule
inhibitor of EGFR, HER2, and VEGFR2, at the 44th Annual Meeting of the
American Society of Clinical Oncology (ASCO). Updated data from an ongoing
phase 2 trial in previously untreated, clinically selected non-small cell
lung cancer (NSCLC) patients show encouraging anti-tumor activity of XL647
administered on an intermittent dosing schedule or a continuous daily
dosing schedule. Additionally, data from a phase 2 trial in patients who
progressed after prior benefit from erlotinib or gefitinib, or who have a
documented EGFR-T790M mutation, also show encouraging signs of activity of
XL647 in this heavily pretreated population. Furthermore, XL647 was
generally well tolerated and showed favorable exposure and tolerability
profiles in a phase 1 trial evaluating daily dosing in patients with
advanced solid tumors.

In this trial, patients with NSCLC were clinically selected on the
basis of adenocarcinoma histology, and either having a documented EGFR
activating mutation in their tumor, or meeting one of the following
criteria: Asian, female, or minimal smoking history. Approximately 30% of
the patients analyzed had EGFR activating mutations. A total of 41 patients
were treated with 350 mg of XL647 on an intermittent (5 days on/9 days off)
dosing schedule, while 8 patients were treated with 300 mg of XL647 on a
daily dosing schedule.

Consistent with data from this phase 2 trial reported in October 2007
at the AACR-NCI-EORTC International Conference on Molecular Targets and
Cancer Therapeutics, the results showed that 27 of 38 evaluable patients
(71%) on the intermittent dosing schedule experienced disease control in
response to treatment with XL647, with 10 partial responses and 17 patients
experiencing stable disease for at least 2 months. All 9 patients with
activating EGFR mutations experienced disease control, with 7 partial
responses and 2 patients with stable disease. In addition, 8 patients
without detectable EGFR mutations also experienced disease control, with 3
partial responses and 5 patients with stable disease. The median
progression-free survival was 9.1 months for patients with activating EGFR
mutations, and 3.8 months for patients without detectable EGFR mutations.

Only 3 of 8 patients in the daily dosing cohort were evaluable for
response as of May 12, 2008. With at least one baseline assessment, 2
patients (1 with an activating EGFR mutation) experienced a partial
response, and 1 patient experienced progressive disease. XL647 was
generally well tolerated in this patient population, with diarrhea,
fatigue, rash, and nausea being the most frequently reported adverse
events. Clinically asymptomatic QTc prolongation was also observed in the
trial.

The data from this trial were presented in a poster session on Sunday,
June 1, 2008 (Abstract #8053).

Phase 2 Trial of XL647 in NSCLC Patients Who Have Progressed After
Prior Benefit from Erlotinib or Gefitinib

XL647 was administered once daily at a dose of 300 mg to patients who
progressed after prior benefit from erlotinib or gefitinib, or who have a
documented EGFR T790M mutation, which is known to confer resistance to
those agents in the clinic. The trial enrolled 41 patients and is now
closed. The results show that 20 of 39 evaluable patients (51%) experienced
disease control (1 partial response and 19 patients with stable disease) in
response to treatment with XL647. In addition, 27% of the patients analyzed
had an EGFR T790M mutation, indicating that the clinical selection of
patients who relapsed after prior benefit from gefitinib or erlotinib
results in a population enriched for this mutation. Three of the 10
patients with the EGFR T790M mutations experienced stable disease in
response to treatment with XL647.

XL647 was generally well tolerated in this patient population, with
diarrhea, fatigue, and rash being the most common adverse events.
Clinically asymptomatic QTc prolongation was also observed in the trial.
Eight patients remain on treatment, while 33 have gone off treatment: 27
due to progressive disease, 5 due to an adverse event, and 1 due to
withdrawn consent.

The data from this trial were presented in a poster discussion session
on Monday, June 2, 2008 (Abstract #8028).

Preliminary results of this ongoing trial show that XL647 is generally
well tolerated at doses up to 300 mg daily. The trial included 31 patients
with advanced solid tumors not amenable to standard therapies. A maximum
tolerated dose (MTD) of 300 mg administered orally once daily was
established. As of May 9, 2008, 16 of 30 evaluable patients (53%) achieved
stable disease with >3 months duration.

Patients received escalating dose levels of XL647 (75 mg-350 mg)
administered orally once daily, and three dose-limiting toxicities (DLTs)
were observed. Two of 4 patients enrolled at 350 mg experienced DLTs of
clinically asymptomatic Grade 3 QTc prolongation that were subsequently
downgraded to Grade 2 following digital analysis by central review. These
patients were dose-reduced to 300 mg daily and did not experience any
further DLTs. One event of Grade 3 drug-induced pneumonitis occurred in 1
patient enrolled at 300 mg. The most common treatment-related adverse
events were diarrhea, rash, dysgeusia, and fatigue. Four patients
experienced a maximum of Grade 1 asymptomatic QTc prolongation as assessed
using digital analysis by a central laboratory, and 11 patients experienced
a maximum of Grade 2.

Preliminary pharmacokinetic data indicate that exposure to XL647
increased approximately in proportion to dose, and that XL647 accumulated
~4.2-fold with repeated daily dosing, with steady state being reached by
approximately Day 15. The XL647 exposure with daily dosing at the MTD (300
mg) in this trial was approximately two-fold higher over a 28-day cycle
compared to the exposure observed previously at the MTD (350 mg) for the
intermittent dosing regimen.

The data from this trial were presented in a poster discussion session
on Saturday, May 31, 2008 (Abstract #3528).

"We continue to be encouraged by the activity of XL647 in the
front-line setting in NSCLC patients clinically selected to enrich for EGFR
activating mutations," said Michael Morrissey, PhD, President of Research
and Development at Exelixis. "We plan to initiate a phase 2 trial of XL647
in untreated NSCLC patients with documented EGFR activating mutations
and/or EGFR gene amplification to further explore the anti-tumor activity
in this patient population. Pending the outcome of this phase 2 trial, we
hope to initiate a pivotal trial in first-line, molecularly-selected NSCLC
patients in the second half of 2009."

Investor and Analyst Briefing at ASCO, Monday, June 2, 6 pm

Exelixis will host an investor and analyst briefing on Monday, June 2,
at 6:00 p.m. at the Hyatt McCormick Place (Regency C&D - 2nd Floor). At
this event, Exelixis will provide a review of its data presented at ASCO
and describe additional data on XL147, a PI3K inhibitor, and XL281, an
inhibitor of RAF. The event will be webcast and may be accessed in the
Event Calendar page under Investors at http://www.exelixis.com. An archived
replay of this webcast will be available until 9:00 p.m. PT/12:00 a.m. ET
on July 2, 2008. Access numbers for this replay are: 1-888-286-8010
(domestic) and +1-617-801-6888 (international); the replay passcode is:
42662164.

About XL647

XL647 inhibits EGFR, HER2, and VEGFR2, which are key targets implicated
in tumor growth and angiogenesis. The compound has been optimized for high
potency and oral bioavailability, demonstrated excellent activity in
target-specific cellular functional assays, and shown sustained inhibition
of target receptor tyrosine kinases (RTKs) in vivo in preclinical models
following a single oral dose. XL647 demonstrated potent inhibition of tumor
growth and caused tumor regression in a broad array of preclinical tumor
models, including breast, lung, colorectal, and prostate cancer. In cell
culture and preclinical tumor models, XL647 retains significant potency
against EGFR mutants, including T790M, which is associated with resistance
to current EGFR inhibitors such as erlotinib and gefitinib. In addition,
XL647 retains activity against a broad spectrum of HER2/ErbB2 mutants that
are resistant to lapatinib.

About Exelixis

Exelixis, Inc. is a development-stage biotechnology company dedicated
to the discovery and development of novel small molecule therapeutics for
the treatment of cancer and other serious diseases. The company is
leveraging its fully integrated drug discovery platform to fuel the growth
of its development pipeline, which is primarily focused on cancer.
Currently, Exelixis' broad product pipeline includes investigational
compounds in phase 2 and phase 1 clinical development. Exelixis has
established strategic corporate alliances with major pharmaceutical and
biotechnology companies, including GlaxoSmithKline, Bristol-Myers Squibb,
Genentech, Wyeth Pharmaceuticals, and Daiichi-Sankyo. For more information,
please visit the company's web site at http://www.exelixis.com.

Forward-Looking Statements

This press release contains forward-looking statements, including
without limitation statements related to the future development and
potential efficacy of XL647 and the timing of the initiation of clinical
trials for XL647. Words such as "hope," "plan," "continue," and similar
expressions are intended to identify forward-looking statements. These
forward-looking statements are based upon our current plans, assumptions,
beliefs and expectations. Forward-looking statements involve risks and
uncertainties. Our actual results and the timing of events could differ
materially from those anticipated in such forward-looking statements as a
result of these risks and uncertainties, which include, without limitation,
risks related to the potential failure of XL647 to demonstrate safety and
efficacy in clinical testing, our ability to initiate and complete clinical
trials for XL647 at the referenced times; the timing and level of expenses
associated with the growth of proprietary programs and other
collaborations; the therapeutic and commercial value of XL647 and our other
compounds; our relationship with our partners; and our ability to enter
into new collaborations, continue existing collaborations and receive
milestones and royalties under our collaborative agreements. These and
other risk factors are discussed under "Risk Factors" and elsewhere in our
quarterly report on Form 10-Q for the quarter ended March 28, 2008, and
other filings with the Securities and Exchange Commission. We expressly
disclaim any duty, obligation or undertaking to release publicly any
updates or revisions to any forward-looking statements contained herein to
reflect any change in our expectations with regard thereto or any change in
events, conditions or circumstances on which any such statements are based.

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